The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
sponsored
Antibacterial.
Pharmacology:Rocephin sodium is a β-lactam antibiotic from the 3rd generation cephalosporin group.
Rocephin is a broad-spectrum cephalosporin antibiotic resistant to β-lactamases. It is active against gram-positive aerobes (Staphylococcus metis, Streptococcus, Streptococcus pneumoniae), gram-negative aerobes (Borrelia burgdorferi, Branhamella catarrhalis, Citrobacter freundii, Citrobacter koseri, Enterobacter, Escherichia coli, Haemophilus influenzae, Klebsiella, Morganella morganii, Neisseria including N. meningitidis and N. gonorrheae, Proteus mirabilis, Proteus multocida, Proteus vulgaris, Providencia, Salmonella, Serratia, Shigella, Yersinia) and anaerobes (Clostridium perfringens, Fusobacterium, Peptostreptococcus, Prevotella).
Pharmacokinetics: Distribution: After IV infusion of a single dosage of 1 g, the maximum serum concentration is in average about 168 mg/L after 30 min. After IM injection of the same dosage, a serum peak of 80 mg/L is reached within 2 or 3 hrs.
The IM and IV routes are bioequivalent (similar areas under the curve). Rocephin administered by IM route has an absolute bioavailability near 100%. The distribution volume of Rocephin is 7-12 L. The diffusion of Rocephin is good in the interstitial liquid, the tissues and the organic liquids (especially the cerebrospinal fluid, bile, bones, bronchial secretions, infectious areas of the ENT sphere).
Protein-Binding: The binding of Rocephin to serum proteins (albumin) is reversible and saturable. It may vary from 80-95% in the range of therapeutic concentrations. As the albumin rate is lower, the proportion of free Rocephin in the interstitial liquid is consequently higher than in the plasma.
Metabolism: Rocephin is very poorly metabolized. The intestinal flora only transforms it to inactive metabolites.
Excretion: Rocephin is excreted by urinary and biliary routes. The total serum clearance is 10-22 mL/min. The renal clearance is 5-12 mL/min. Fifty to 60% of Rocephin is excreted as unchanged form in the urine whereas around 40-50% is excreted in the bile. In adults, the elimination t½ is about 8 hrs long.
Pharmacokinetics in Particular Clinical Conditions: In newborns, the quantity of Rocephin remaining in the urine corresponds to about 70% of the administered dosage.
In newborns <8 days, the average elimination t½ is generally 2 or 3 times higher than in young adults; it is shorter in newborns 3-12 months.
In children and newborns, after a single IM injection of 50 mg/kg, the peak serum concentration of Rocephin is reached after 5.4 hrs (192±135mg/L).
In children and newborns, after a single IM injection, the diffusion in the middle ear is good with rates higher than the MIC of main bacillus responsible for middle ear acute disease during at least 48 hrs. After a single injection of 50 mg/kg, the total concentration of Rocephin in the middle ear liquid is about 5 mg/L after 1.5 hrs (33±20 mg/L), after the 15th hr, stable on the 24th hr (35±12 mg/L) and is still about 19±7mg/L after 48 hrs.
In patients with renal or hepatic insufficiency, Rocephin pharmacokinetics is very much different and the elimination t½ is only very poorly increased. If only the renal function is concerned, then the Rocephin biliary elimination is increased. If only the hepatic function is concerned, the renal elimination is increased.
How should I take Rocephin?
A nurse or other trained health professional will give you Rocephin. Rocephin is given as a shot into one of your muscles or through a needle placed in one of your veins.
Rocephin administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
sponsored
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Rocephin is injected into a muscle, or into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.
Rocephin must be given slowly, and the IV infusion can take at least 30 minutes to complete.
You may need to mix Rocephin with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medication. Use only the diluent your doctor has recommended.
After mixing your medicine, you will need to use it within a certain number of hours or days. This will depend on the diluent and how you store the mixture (at room temperature, in a refrigerator, or frozen). Carefully follow the mixing and storage instructions provided with your medicine. Ask your pharmacist if you have questions.
Do not mix Rocephin in the same injection with other antibiotics, or with any diluent that contains calcium, including a TPN (total parenteral nutrition) solution.
If you use other injectable medications, be sure to flush your intravenous catheter between injections of each medication.
Use this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Rocephin will not treat a viral infection such as the common cold or flu.
This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Rocephin.
Store unmixed Rocephin powder at room temperature, away from moisture, heat, and light.
If your medicine was provided in a frozen form or was frozen after mixing, thaw it in a refrigerator or at room temperature. Do not warm in a microwave or boiling water. Use the medicine as soon as possible after thawing it. Do not refreeze.
Rocephin pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
sponsored
Average plasma concentrations of Rocephin (Rocephin sodium and dextrose injection ) following a single 30-minute intravenous (IV) infusion of a 0.5,1 or 2 g dose in healthy subjects are presented in Table 1.
TABLE 1. Rocephin (Rocephin sodium and dextrose injection ) Plasma Concentrations After Single Dose Administration
Dose/Route
Average Plasma Concentrations (µ/mL)
0.5 hr
1 hr
2hr
4hr
6hr
8hr
12hr
16 hr
24 hr
0.5 g IV*
82
59
48
37
29
23
15
10
5
1 g IV*
151
111
88
67
53
43
28
18
9
2 g IV*
257
192
154
117
89
74
46
31
15
*IV doses were infused at a constant rate over 30 minutes.
Multiple IV doses ranging from 0.5 to 2 g at 12- to 24-hour intervals resulted in 15% to 36% accumulation of Rocephin (Rocephin sodium and dextrose injection ) above single dose values.
Rocephin (Rocephin sodium and dextrose injection ) concentrations in urine are high, as shown in Table 2.
TABLE 2. Urinary Concentrations of Rocephin (Rocephin sodium and dextrose injection ) After Single Dose Administration
Dose/Route
Average Urinary Concentrations (µ/mL)
0-2 hr
2-4 hr
4-8 hr
8-12 hr
12-24 hr
24-48 hr
0.5 g IV
526
366
142
87
70
15
1 g IV
995
855
293
147
132
32
2g lV
2692
1976
757
274
198
40
Thirty-three percent to 67% of a Rocephin (Rocephin sodium and dextrose injection ) dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. After a 1 g IV dose, average concentrations of Rocephin (Rocephin sodium and dextrose injection ), determined from 1 to 3 hours after dosing, were 581 µg/mL in the gallbladder bile, 788 µglml in the common duct bile, 898 µg/mL in the cystic duct bile, 78.2 µg/g in the gallbladder wall and 62.1 µg/mL in the concurrent plasma.
Over a 0.15 to 3 g dose range in healthy adult subjects, the values of elimination half-life ranged from 5.8 to 8.7 hours; apparent volume of distribution from 5.78 to 13.5 L; plasma clearance from 0.58 to 1.45 L/hour; and renal clearance from 0.32 to 0.73 L/hour. Rocephin (Rocephin sodium and dextrose injection ) is reversibly bound to human plasma proteins, and the binding decreased from a value of 95% bound at plasma concentrations of < 25 µg/mL to a value of 85% bound at 300 µg/mL. Rocephin (Rocephin sodium and dextrose injection ) crosses the blood placenta barrier.
The average values of maximum plasma concentration, elimination half-life, plasma clearance and volume of distribution after a 50 mg/kg IV dose and after a 75 mg/kg IV dose in pediatric patients suffering from bacterial meningitis are shown in Table 3. Rocephin (Rocephin sodium and dextrose injection ) penetrated the inflamed meninges of infants and pediatric patients; CSF concentrations after a 50 mg/kg IV dose and after a 75 mg/kg IV dose are also shown in Table 3.
TABLE 3. Average Pharmacokinetic Parameters of Rocephin (Rocephin sodium and dextrose injection ) in Pediatric Patients With Meningitis
50 mg/kg IV
75 mg/kq IV
Maximum Plasma Concentrations (µg/mL)
216
275
Elimination Half-life (hr)
4.6
4.3
Plasma Clearance (mL/hr/kg)
49
60
Volume of Distribution (mL/kg)
338
373
CSF Concentration — inflamed meninges (µg/mL)
5.6
6.4
Range (µ/mL)
1.3-18.5
1.3-44
Time after dose (hr)
3.7 (±1.6)
3.3 (±1.4)
Compared to that in healthy adult subjects, the pharmacokinetics of Rocephin (Rocephin sodium and dextrose injection ) were only minimally altered in elderly subjects and in patients with renal impairment or hepatic dysfunction (Table 4); therefore, dosage adjustments are not necessary for these patients with Rocephin (Rocephin sodium and dextrose injection ) dosages up to 2 g per day. Rocephin (Rocephin sodium and dextrose injection ) was not removed to any significant extent from the plasma by hemodialysis. In 6 of 26 dialysis patients, the elimination rate of Rocephin (Rocephin sodium and dextrose injection ) was markedly reduced, suggesting that plasma concentrations of Rocephin (Rocephin sodium and dextrose injection ) should be monitored in these patients to determine if dosage adjustments are necessary.
TABLE 4. Average Pharmacokinetic Parameters of Rocephin (Rocephin sodium and dextrose injection ) in Humans
Subject Group
Elimination
Half-Life
(hr)
Plasma
Clearance
(L/hr)
Volume of
Distribution
(L)
Healthy Subjects
5.8-8.7
0.58-1.45
5.8-13.5
Elderly Subjects (mean age, 70.5 yr)
8.9
0.83
10.7
Patients with Renal Impairment
Hemodialysis Patients (0-5 mL/min)*
14.7
0.65
13.7
Severe (5-15 mL/min)
15.7
0.56
12.5
Moderate (16-30 mL/min)
11.4
0.72
11.8
Mild (31-60 mL/min)
12.4
0.70
13.3
Patients With Liver Disease
8.8
1.1
13.6
*Creatinine clearance.
Microbiology
The bactericidal activity of Rocephin (Rocephin sodium and dextrose injection ) results from inhibition of cell wall synthesis. Rocephin (Rocephin sodium and dextrose injection ) has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria.
Rocephin (Rocephin sodium and dextrose injection ) has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections described in the INDICATIONS AND USAGE section.
Aerobic gram-negative microorganisms
Acinetobacter calcoaceticus
Enterobacter aerogenes
Enterobacter cloacae
Escherichia coli
Haemophilus influenzae (including ampicillin-resistant and beta-lactamase producing strains)
Neisseria gonorrhoeae (including penicillinase- and nonpenicillinase-producing strains)
Neisseria meningitidis
Proteus mirabilis
Proteus vulgaris
Serratia marcescens
Rocephin (Rocephin sodium and dextrose injection ) is also active against many strains of Pseudomonas aeruginosa.
NOTE: Many strains of the above organisms that are multiply resistant to other antibiotics, e.g., penicillins, cephalosporins, and aminoglycosides, are susceptible to Rocephin (Rocephin sodium and dextrose injection ).
NOTE: Methicillin-resistant staphylococci are resistant to cephalosporins, including Rocephin (Rocephin sodium and dextrose injection ). Most strains of Group D streptococci and enterococci, e.g., Enterococcus (Streptococcus) faecalis, are resistant.
Anaerobic microorganisms
Bacteroides fragilis
Clostridium species
Peptostreptococcus species
NOTE: Most strains of Clostridium difficile are resistant.
The following in vitro data are available, but their clinical significance is unknown. Rocephin (Rocephin sodium and dextrose injection ) exhibits in vitro minimal inhibitory concentrations (MICs) of ≤ 8 µg/mL or less against most strains of the following microorganisms, however, the safety and effectiveness of Rocephin (Rocephin sodium and dextrose injection ) in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.
Aerobic gram-negative microorganisms
Citrobacter diversus
Citrobacterfreundii
Providencia species (including Providencia rertgeri)
Salmonella species (including Salmonella typhi)
Shigella species
Aerobic gram-positive microorganisms
Streptococcus agalactiae
Anaerobic microorganisms
Prevotella (Bacteroides) bivius
Porphyromonas (Bacteroides) melaninogenicus
Susceptibility Tests
Dilution Techniques
Quantitative methods are used to determine antimicrobial minimal inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized procedure. testing method:
Method
Microoraanism
ATCC®#
MIC (µq/mL)
Agar
Bacteroides fragilis
25285
32-128
Bacteroides thetaiotaomicron
29741
64-256
Broth
Bacteroides thetaiotaomicron
29741
32-128
REFERENCES
1. National Committee for Clinical Laboratory Standards, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically; Approved Standard-Fifth Edition. NCCLS document M7-A5 (ISBN 1-56238-309-9). NCCLS, Wayne, PA 19087-1898,2000.
2. National Committee for Clinical Laboratory Standards, Supplemental Tables. NCCLS document M100-S10(M7) (ISBN 1-56238-309-9). NCCLS, Wayne, PA 19087-1898,2000.
3. National Committee fof'Clinical Laboratory Standards, Performance Standards for Antimicrobial Disk Susceptibility Teste; Approved Standard-Seventh Edition. NCCLS document M2-A7 (ISBN 1-56238-393-0). NCCLS, Wayne, PA 19087-1898,2000.
4. National Committee for Clinical Laboratory Standards, Methods for Antimicrobial Susceptibility Testing of Anaerobic Bacterial; Approved Standard-Fourth Edition. NCCLS document M11-A4 (ISBN 1-56238-210-1). NCCLS, Wayne, PA 19087-1898,1997.
References
DailyMed. "CEFTRIAXONE SODIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
NCIt. "Ceftriaxone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
NCIt. "Cefuroxime: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Rocephin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Rocephin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
User reports
1 consumer reported administration
When best can I take Rocephin, on an empty stomach, before or after food? ndrugs.com website users have also released a report stating that Rocephin should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Rocephin. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Rocephin can be taken.
Users
%
Empty stomach
1
100.0%
Consumer reviews
There are no reviews yet. Be the first to write one!
